| Stereochemistry | ACHIRAL |
| Molecular Formula | C12H16N2O2 |
| Molecular Weight | 220.2676 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
C1CN(CCN1)C2=CC=CC3=C2OCCO3
InChI
InChIKey=WVLHGCRWEHCIOT-UHFFFAOYSA-N
InChI=1S/C12H16N2O2/c1-2-10(14-6-4-13-5-7-14)12-11(3-1)15-8-9-16-12/h1-3,13H,4-9H2
| Molecular Formula | C12H16N2O2 |
| Molecular Weight | 220.2676 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
Eltoprazine, a 5-HT1A/B receptor partial agonist, was created by Duphar in the 1980s (as DU-28853) and was subsequently developed by Solvay to treat pathological aggression. This drug is in clinical development for the treatment of Parkinson's disease levodopa-induced dyskinesia (PD-LID), Alzheimer's aggression and adult attention deficit hyperactivity disorder (adult ADHD). In addition, was shown, that the drug could be useful for normalizing prefrontal cognitive abilities, reducing aggression and impulsivity, and improving cognitive function in schizophrenia.
Originator
Approval Year
PubMed
Patents
Sample Use Guides
eltoprazine HCl 2.5; 5 or 7.5 mg capsules to be taken orally b.i.d. (ie, 5 mg/day) for 3 weeks
Route of Administration:
Oral
There was localized and characterized the binding sites of [3H]eltoprazine in the rat brain. The binding of [3H]eltoprazine to whole tissue sections was saturable and revealed an apparent dissociation constant (Kd) of 11 nM. Autoradiographic studies demonstrated a widespread distribution of [3H]eltoprazine binding sites throughout the brain. Specific [3H]eltoprazine binding was completely displaced by 5-HT; conversely, unlabeled eltoprazine reduced [3H]5-HT binding to the levels of non-specific binding. The pharmacological and anatomical data indicate that eltoprazine binds to 5-HT1A, 5-HT1B and to a lesser extent to 5-HT1C binding sites in the rat brain.
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SALT/SOLVATE -> PARENT |
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